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Compound Detail

CHEMBL471261

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COc1cc(C(=O)NCCN2CCC3(CC2)C(=O)NCN3c2ccccc2)ccc1N

Basic Information

ChEMBL ID CHEMBL471261
Phase Preclinical
Structure Type MOL
InChI Key PHTMXPVDOTYOPK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

423.5
MW (Da)
1.44
ALogP
6
HBA
3
HBD
99.9
PSA (Ų)
0.61
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H29N5O3
MW 423.52
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.86

Activity Summary

IC50 2 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phospholipase D2
CHEMBL2734
IC50 6.26 6.26 550.0 1
Phospholipase D1
CHEMBL2536
IC50 5.23 5.23 5900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phospholipase D2 IC50 = 550.0 nM 6.26 Inhibition of GFP-labeled PLD2 in human HEK293 cells 19299128
Phospholipase D1 IC50 = 5900.0 nM 5.23 Inhibition of PLD1 in human Calu1 cells 19299128

Literature References

PubMed DOI Target Context # Activities
19299128 10.1016/j.bmcl.2009.02.125 Phospholipase D1 1
19299128 10.1016/j.bmcl.2009.02.125 Phospholipase D2 1
19299128 10.1016/j.bmcl.2009.02.125 Unchecked 1

Data from ChEMBL 36 via Core Engine